EP0063132A1 - New galenical administration form of metoclopramide, method for its preparation and medicament comprising this new form. - Google Patents
New galenical administration form of metoclopramide, method for its preparation and medicament comprising this new form.Info
- Publication number
- EP0063132A1 EP0063132A1 EP81902835A EP81902835A EP0063132A1 EP 0063132 A1 EP0063132 A1 EP 0063132A1 EP 81902835 A EP81902835 A EP 81902835A EP 81902835 A EP81902835 A EP 81902835A EP 0063132 A1 EP0063132 A1 EP 0063132A1
- Authority
- EP
- European Patent Office
- Prior art keywords
- metoclopramide
- microgranules
- new
- neutral
- weight
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
- A61K9/5078—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings with drug-free core
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
Definitions
- METOCLOPRAMIDE has been known for many years. In the form of dihydrochloride or monohydrochloride, it is widely used to treat functional gastrointestinal disturbances such as dyspepsia, peptic and biliary dyskinesia, chronic gastritis, peptic ulcers, nausea and vomiting. Pharmacologically, the action of METOCLOPRAMIDE is both central and peripheral. However, the administration of METOCLOPRAMIDE in its current form has significant drawbacks, limiting the convenience of use.
- the present invention therefore relates to a new dosage form with delayed programmed release of METOCLOPRAMIDE and is characterized in that it is constituted by microgranules comprising a neutral core consisting of a grain of an inert excipient comprising at least two components of the type belonging to the class consisting of sucrose, starch, talc, drying silica, lactose and stearic acid, this neutral grain being provided with a first layer comprising METOCLOPRAMIDE, then with a second outer layer consisting of a microporous envelope comprising at least one natural and / or synthetic polymer belonging to the class consisting of shellac, gum arabic, gelatin, ethylcellulose, cellulose acetophthalate, cellulose triacetate, polyoxyethylene glycol, methacrylates, styrene-acrylonitrile copolymer and polyvinylpyrrolidone in successive envelopes.
- a neutral core consisting of a grain of an inert excipient comprising at
- the microporous envelope can be formed of shellac in a proportion by weight varying between 1 and 10%
- the inert excipient can be a mixture comprising from 40 to 80% by weight of sucrose and from 10 to 40%. by weight of starch.
- the first layer may comprise from 1 to 20% by weight of METOCLOPRAMIDE, from 0.01% to 0.5% by weight of stearic acid, from 5 to 15% by weight talc and 2 to 10% by weight of drying silica.
- the neutral core may include adsorbates of METOCLOPRAMIDE.
- the subject of the invention is also a process for obtaining the remarkable new galenical form in that neutral sieved and dried microgranules are prepared beforehand, that a solution in absolute alcohol of METOCLOPRAMIDE is projected onto these microgranules, then coating said microgranules to make the first layer in one or more coatings, then forming the microporous envelope by coating with said polymer in solution in a solvent.
- the present invention relates to medicaments comprising the new form of administration of METOCLOPRAMIDE in the form of active microgranules mixed with neutral uncoated microgranules in order to obtain a predetermined concentration of METOCLOPRAMIDE, this set of microgranules being presented in the form capsules, tablets, suppositories, syrup, granules or powder.
- METOCLOPRAMIDE The first layer is then made by incorporating the other excipients with the exception of shellac into these microgranules, then the spraying of METOCLOPRAMIDE hydrochloride is restarted, this coating being repeated several times with sieving and drying if necessary between each layer.
- the microporous outer layer is produced by spraying the shellac with the granules in solution in absolute ethyl alcohol.
- microporous outer envelope is made so as to allow a prolonged release of theoretical METOCLOPRAMIDE:
- a disintegration device in which an amount of microgranules corresponding to approximately 50 mg of contact is brought into contact.
- active principle with artificial liquids the device making it possible to maintain constant agitation and a constant temperature of 37 ° ⁇ 0.5 ° C.
- Artificial liquids are solutions buffered at successive pH used according to the diagram below.
- the new dosage form according to the invention was the subject of an in-depth pharmacokinetic study in comparison with the conventional tablet form.
- the study was carried out in cross-over in humans.
- Six male subjects received each of the two forms at two-week intervals, one 20 mg capsule of active ingredient containing the microgranules and two 10 mg tablets of the conventional form.
- the plasma concentration of METOCLOPRAMIDE was determined by means of 10 samples in the interval of 72 hours.
- the time of appearance of the serum peak increases from 1 hour to 4.5 hours.
- the half-life duration increases from approximately 3 hours to more than 8 hours.
- the new dosage presentation leads to a new drug useful for the treatment of gastric disorders in general.
- FIGURE 1 Plasma concentrations of METOCLOPRAMIDE after an oral cross-over dose in 6 subjects . are healthy
- FIGURE 2 Plasma concentrations of METOCLOPRAMIDE after an oral dose taken in cross-over in 6 healthy subjects
- FIGURE 3 METOCLOPRAMIDE plasma concentrations
Landscapes
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Medicament a base de metoclopramide presente sous une nouvelle forme galenique a effet retard. Le principe actif contenu dans des microgranules inclus dans une gelule est libere progressivement. Le nouveau medicament permet de diminuer le nombre de prises journalieres et de reduire la quantite de principe actif ingere.Metoclopramide-based drug in a new dosage form with a delayed effect. The active ingredient contained in microgranules included in a capsule is gradually released. The new drug makes it possible to reduce the number of daily intakes and to reduce the quantity of active ingredient ingested.
Description
Claims
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR8023028A FR2492661A1 (en) | 1980-10-28 | 1980-10-28 | NOVEL GALENIC FORM OF ADMINISTRATION OF METOCLOPRAMIDE, ITS PREPARATION METHOD AND MEDICINAL PRODUCT COMPRISING THIS NOVEL FORM |
FR8023028 | 1980-10-28 |
Publications (2)
Publication Number | Publication Date |
---|---|
EP0063132A1 true EP0063132A1 (en) | 1982-10-27 |
EP0063132B1 EP0063132B1 (en) | 1986-07-30 |
Family
ID=9247410
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP81902835A Expired EP0063132B1 (en) | 1980-10-28 | 1981-10-22 | New galenical administration form of metoclopramide, method for its preparation and medicament comprising this new form |
Country Status (13)
Country | Link |
---|---|
US (1) | US4656024A (en) |
EP (1) | EP0063132B1 (en) |
JP (1) | JPH0428685B2 (en) |
AU (1) | AU555512B2 (en) |
BE (1) | BE890808A (en) |
CA (1) | CA1166574A (en) |
CH (1) | CH650922A5 (en) |
ES (1) | ES8301633A1 (en) |
FR (1) | FR2492661A1 (en) |
GR (1) | GR74683B (en) |
IT (1) | IT1139645B (en) |
WO (1) | WO1982001468A1 (en) |
ZA (1) | ZA816993B (en) |
Families Citing this family (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2534139B1 (en) * | 1982-10-07 | 1986-08-29 | Laruelle Claude | NOVEL GALENIC FORM OF SULPIRIDE, METHOD FOR PREPARING SAME, AND MEDICINAL PRODUCT COMPRISING THIS NEW FORM |
FR2539995B1 (en) * | 1983-01-28 | 1985-08-16 | Sanofi Sa | PROGRAMMED RELEASE MEDICINE BASED ON ACETYLSALICYLIC ACID |
FR2556964A1 (en) * | 1983-12-23 | 1985-06-28 | Ile De France | NEW GALENIC FORMS OF SULPIRIDE USED ORALALLY |
DE3403329A1 (en) * | 1984-02-01 | 1985-08-01 | Horst Dr. 4019 Monheim Zerbe | PHARMACEUTICAL PRODUCT IN THE FORM OF PELLETS WITH CONTINUOUS, DELAYED DELIVERY OF ACTIVE SUBSTANCES |
GB8412585D0 (en) * | 1984-05-17 | 1984-06-20 | Beecham Group Plc | Composition |
IT1176853B (en) * | 1984-10-02 | 1987-08-18 | Eurand Spa | PROCEDURE FOR OBTAINING A CONTROLLED RELEASE FORMULATION OF WATER SOLUBLE COMPONENTS |
JPS6261916A (en) * | 1985-09-12 | 1987-03-18 | Fujisawa Pharmaceut Co Ltd | Long-acting drug |
LU86077A1 (en) * | 1985-09-18 | 1987-04-02 | Pharlyse Sa | NEW GALENIC FORMS OF VERAPAMIL, THEIR MANUFACTURE AND THE MEDICINAL PRODUCTS CONTAINING THESE NEW GALENIC FORMS |
DE3712095A1 (en) * | 1987-04-10 | 1988-10-20 | Lentia Gmbh | BINDER-FREE GRANULES WITH DELAYED DELIVERY OF ACTIVE SUBSTANCES |
DE4131276B4 (en) * | 1990-09-28 | 2007-07-19 | Solvay Pharmaceuticals Gmbh | Perorally administrable metoclopramide solutions |
US5286495A (en) * | 1992-05-11 | 1994-02-15 | University Of Florida | Process for microencapsulating cells |
EP1202745A4 (en) * | 1999-08-16 | 2004-09-22 | Henceforth Hibernia Inc | Therapeutic and prophylactic compositions including catalytic biomimetic solids and methods to prepare and use them |
ATE376826T1 (en) * | 2001-09-28 | 2007-11-15 | Mcneil Ppc Inc | MODIFIED RELEASE PHARMACEUTICAL FORMS |
MX2008004268A (en) * | 2008-03-28 | 2009-09-28 | Posi Visionary Solutions Llp | 24-hour sustained-release metoclopramide. |
MX2008004267A (en) * | 2008-03-28 | 2009-09-28 | Posi Visionary Solutions Llp | 24-hour sustained-release metoclopramide. |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2963402A (en) * | 1955-01-18 | 1960-12-06 | Nysco Lab Inc | Sustained release medicament |
FR1347413A (en) * | 1963-01-29 | 1963-12-27 | Italnysco S P A | Broad-acting spherules or globules and method for their preparation |
BE787973A (en) * | 1971-09-04 | 1973-02-26 | Beecham Group Ltd | DELAY-EFFECT PHARMACEUTICAL TABLETS |
FR2313915A1 (en) * | 1976-01-26 | 1977-01-07 | Corneille Gilbert | Sustained release vincamine microcapsules - with inert core, vincamine (deriv.) intermediate layer and microporous outer coating |
LU77353A1 (en) * | 1977-05-16 | 1979-01-19 | ||
FR2397840B1 (en) * | 1977-07-22 | 1981-03-20 | Cherqui Jean | |
FR2432313A1 (en) * | 1978-08-01 | 1980-02-29 | Foulhoux Pierre | Micro:granules contg. beta-histine - for controlled release and less side effects useful in treating Menieres syndrome |
BE876857A (en) * | 1979-06-08 | 1979-10-01 | Trenker Ady | METOCLOPRAMIDE RESINATE. |
-
1980
- 1980-10-28 FR FR8023028A patent/FR2492661A1/en active Granted
-
1981
- 1981-10-09 ZA ZA816993A patent/ZA816993B/en unknown
- 1981-10-21 BE BE1/10338A patent/BE890808A/en not_active IP Right Cessation
- 1981-10-21 IT IT24601/81A patent/IT1139645B/en active
- 1981-10-22 US US06/607,401 patent/US4656024A/en not_active Expired - Fee Related
- 1981-10-22 JP JP56503317A patent/JPH0428685B2/ja not_active Expired - Lifetime
- 1981-10-22 EP EP81902835A patent/EP0063132B1/en not_active Expired
- 1981-10-22 AU AU77204/81A patent/AU555512B2/en not_active Ceased
- 1981-10-22 WO PCT/FR1981/000134 patent/WO1982001468A1/en active IP Right Grant
- 1981-10-23 CA CA000388666A patent/CA1166574A/en not_active Expired
- 1981-10-26 GR GR66362A patent/GR74683B/el unknown
- 1981-10-27 CH CH6860/81A patent/CH650922A5/en not_active IP Right Cessation
- 1981-10-28 ES ES506654A patent/ES8301633A1/en not_active Expired
Non-Patent Citations (1)
Title |
---|
See references of WO8201468A1 * |
Also Published As
Publication number | Publication date |
---|---|
JPS57502121A (en) | 1982-12-02 |
WO1982001468A1 (en) | 1982-05-13 |
IT1139645B (en) | 1986-09-24 |
FR2492661B1 (en) | 1983-07-18 |
ES506654A0 (en) | 1983-01-01 |
CH650922A5 (en) | 1985-08-30 |
JPH0428685B2 (en) | 1992-05-15 |
EP0063132B1 (en) | 1986-07-30 |
BE890808A (en) | 1982-04-21 |
GR74683B (en) | 1984-07-03 |
ES8301633A1 (en) | 1983-01-01 |
AU555512B2 (en) | 1986-09-25 |
FR2492661A1 (en) | 1982-04-30 |
CA1166574A (en) | 1984-05-01 |
AU7720481A (en) | 1982-05-21 |
IT8124601A0 (en) | 1981-10-21 |
ZA816993B (en) | 1982-09-29 |
US4656024A (en) | 1987-04-07 |
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